Estimation of haloperidol concentrations in rat striatum after chronic treatment

Elisabeth P. Bellows; Deborah E. Barnes; John G. Csernansky

doi:10.1016/0361-9230(91)90165-G

Estimation of haloperidol concentrations in rat striatum after chronic treatment

Elisabeth P. Bellows, Deborah E. Barnes, John G. Csernansky^*

^*Corresponding author for this work

Psychiatry and Behavioral Sciences

Research output: Contribution to journal › Article › peer-review

3 Scopus citations

Abstract

³H-Spiroperidol association and dissociation rate constants were determined in rat striatal homogenates in the presence of known concentrations of unlabelled haloperidol. The rate of ³H-spiroperidol association was progressively decreased in the presence of increasing concentrations of haloperidol and no changes were seen in ³H-spiroperidol dissociation rate constants. Measuring changes in ³H-spiroperidol association rate constants permitted detection of 0.1 pmol/ml unlabelled haloperidol in assay homogenates. Then, male Sprague-Dawley rats received daily injections of haloperidol (1.5 mg/kg) for 1-21 days. Twenty-four hours after the last injection, ³H-spiroperidol kinetic rate constants and K_d values were measured and found to be unchanged in all treatment groups. These findings suggest that, under these conditions of drug withdrawal and tissue preparation, which are widely employed in studies of chronic neuroleptic administration, residual haloperidol does not interfere with the estimation of ³H-spiroperidol binding parameters.

Original language	English (US)
Pages (from-to)	715-719
Number of pages	5
Journal	Brain Research Bulletin
Volume	26
Issue number	5
DOIs	https://doi.org/10.1016/0361-9230(91)90165-G
State	Published - May 1991

Keywords

Dopamine
H-Spiroperidol
Haloperidol
Neuroleptics
Radioreceptor binding assay
Rat striatum

ASJC Scopus subject areas

General Neuroscience

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10.1016/0361-9230(91)90165-G

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title = "Estimation of haloperidol concentrations in rat striatum after chronic treatment",

abstract = "3H-Spiroperidol association and dissociation rate constants were determined in rat striatal homogenates in the presence of known concentrations of unlabelled haloperidol. The rate of 3H-spiroperidol association was progressively decreased in the presence of increasing concentrations of haloperidol and no changes were seen in 3H-spiroperidol dissociation rate constants. Measuring changes in 3H-spiroperidol association rate constants permitted detection of 0.1 pmol/ml unlabelled haloperidol in assay homogenates. Then, male Sprague-Dawley rats received daily injections of haloperidol (1.5 mg/kg) for 1-21 days. Twenty-four hours after the last injection, 3H-spiroperidol kinetic rate constants and Kd values were measured and found to be unchanged in all treatment groups. These findings suggest that, under these conditions of drug withdrawal and tissue preparation, which are widely employed in studies of chronic neuroleptic administration, residual haloperidol does not interfere with the estimation of 3H-spiroperidol binding parameters.",

keywords = "Dopamine, H-Spiroperidol, Haloperidol, Neuroleptics, Radioreceptor binding assay, Rat striatum",

author = "Bellows, {Elisabeth P.} and Barnes, {Deborah E.} and Csernansky, {John G.}",

note = "Funding Information: This work was supportedb y a grant from the Scottish Rite Schizophrenia Research Program, N.M.J., USA, to J.G.C. and E.P.B. and a grant from the Research Service of the Departmento f Veterans Affairs (formerly Veterans Administration) to the Schizophrenia Biologic Research Center (SBRC) at the Department of Veterans Affairs Medical Center, Palo Alto, CA. The authors thank Pamela J. Elliott for manuscript preparationa nd editorial advice.",

year = "1991",

month = may,

doi = "10.1016/0361-9230(91)90165-G",

language = "English (US)",

volume = "26",

pages = "715--719",

journal = "Brain Research Bulletin",

issn = "0361-9230",

publisher = "Elsevier Inc.",

number = "5",

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TY - JOUR

T1 - Estimation of haloperidol concentrations in rat striatum after chronic treatment

AU - Bellows, Elisabeth P.

AU - Barnes, Deborah E.

AU - Csernansky, John G.

N1 - Funding Information: This work was supportedb y a grant from the Scottish Rite Schizophrenia Research Program, N.M.J., USA, to J.G.C. and E.P.B. and a grant from the Research Service of the Departmento f Veterans Affairs (formerly Veterans Administration) to the Schizophrenia Biologic Research Center (SBRC) at the Department of Veterans Affairs Medical Center, Palo Alto, CA. The authors thank Pamela J. Elliott for manuscript preparationa nd editorial advice.

PY - 1991/5

Y1 - 1991/5

N2 - 3H-Spiroperidol association and dissociation rate constants were determined in rat striatal homogenates in the presence of known concentrations of unlabelled haloperidol. The rate of 3H-spiroperidol association was progressively decreased in the presence of increasing concentrations of haloperidol and no changes were seen in 3H-spiroperidol dissociation rate constants. Measuring changes in 3H-spiroperidol association rate constants permitted detection of 0.1 pmol/ml unlabelled haloperidol in assay homogenates. Then, male Sprague-Dawley rats received daily injections of haloperidol (1.5 mg/kg) for 1-21 days. Twenty-four hours after the last injection, 3H-spiroperidol kinetic rate constants and Kd values were measured and found to be unchanged in all treatment groups. These findings suggest that, under these conditions of drug withdrawal and tissue preparation, which are widely employed in studies of chronic neuroleptic administration, residual haloperidol does not interfere with the estimation of 3H-spiroperidol binding parameters.

AB - 3H-Spiroperidol association and dissociation rate constants were determined in rat striatal homogenates in the presence of known concentrations of unlabelled haloperidol. The rate of 3H-spiroperidol association was progressively decreased in the presence of increasing concentrations of haloperidol and no changes were seen in 3H-spiroperidol dissociation rate constants. Measuring changes in 3H-spiroperidol association rate constants permitted detection of 0.1 pmol/ml unlabelled haloperidol in assay homogenates. Then, male Sprague-Dawley rats received daily injections of haloperidol (1.5 mg/kg) for 1-21 days. Twenty-four hours after the last injection, 3H-spiroperidol kinetic rate constants and Kd values were measured and found to be unchanged in all treatment groups. These findings suggest that, under these conditions of drug withdrawal and tissue preparation, which are widely employed in studies of chronic neuroleptic administration, residual haloperidol does not interfere with the estimation of 3H-spiroperidol binding parameters.

KW - Dopamine

KW - H-Spiroperidol

KW - Haloperidol

KW - Neuroleptics

KW - Radioreceptor binding assay

KW - Rat striatum

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SN - 0361-9230

VL - 26

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EP - 719

JO - Brain Research Bulletin

JF - Brain Research Bulletin

IS - 5

ER -

Estimation of haloperidol concentrations in rat striatum after chronic treatment

Abstract

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